Ceritinib-d7 is intended for use as an internal standard for the quantification of ceritinib by GC- or LC-MS. Ceritinib is an inhibitor of anaplastic lymphoma kinase (ALK) with an IC50 value of 200 pM in an enzyme assay.1,2 It less potently inhibits IGF-1R, InsR, and STK22D (IC50s = 8, 7, and 23 nM, respectively) and is minimally effective against a panel of other kinases. Ceritinib inhibits ALK in cells (IC50 = 25 nM) and in vivo, producing tumor regression in a rat xenograft model.1 It is also effective against several crizotinib-resistant mutants of ALK.3
|1. Awad, M.M., and Shaw, A.T. ALK inhibitors in non-small cell lung cancer: Crizotinib and beyond. Clin. Adv. Hematol. Oncol. 12(7), 429-439 (2014).|2. Sullivan, I., and Planchard, D. ALK inhibitors in non-small cell lung cancer: The latest evidence and developments. Ther. Adv. Med. Oncol. 8(1), 32-47 (2016).|3. Fontana, D., Ceccon, M., Gambacorti-Passerini, C., et al. Activity of second-generation ALK inhibitors against crizotinib-resistant mutants in an NPM-ALK model compared to EML4-ALK. Cancer Med. 4(7), 953-965 (2016).